Design and evaluation of flexible membrane vesicles (FMVs) for enhanced topical delivery of capsaicin

Abstract

Capsaicin, extracted from the fruits of Capsicum, is a powerful local stimulant with strong rubifacient action, devoid of vesication. Topical use of capsaicin is quite common in the treatment of various pain-associated musculo-skeletal disorders, itching and neuropathy. Despite its high pharmacodynamic potential, the patient compliance to the drug is reported to be poor owing to multiple skin problems like irritation, burning sensation, and erythma. The present study targets the encasement of drug in the interiors of flexible membrane vesicles (FMVs), as these are reported to have better penetration in the deeper layers of skin, thus leading to enhanced localization of drug and consequently, decreased skin irritation. Multilamellar drug-loaded FMVs, prepared by thin-film hydration were evaluated for their efficacy in vitro and in vivo. When compared with conventional liposomes, the formulated FMVs showed higher skin retention during ex vivo permeation studies employing LACA mice skin, higher analgesic potential using radiant tail-flick method in mice, and better flexibility in regaining their size. Being less of an irritant, these vesicular carriers were also found to be more comfortable on human skin. Thus, the capsaicin-loaded FMVs offer high potential as topical drug delivery technologies with improved patient acceptance and effectiveness.

Systematic Development of Transethosomal Gel System of Piroxicam: Formulation Optimization, In Vitro Evaluation, and Ex Vivo Assessment

“…The method for the preparation of liposomes, transfersomes, and ethosomes was similar to that of transethosomes. The amount of piroxicam, i.e., 500 mg of piroxicam per 100 ml of the formulation, was fixed in all the formulations, and the amount of Span 80 was fixed according to the ratio of SPL 70 and Span 80 (5,24,25). The composition for these formulations is shown in Table IV.…”

“…The column was eluted four times with 0.2 ml distilled water. These eluted vesicles were digested, ruptured with methanol, and analyzed spectrophotometrically at 365 nm (5,8,27 …”

“…The processed skin was sonicated for 20 m and centrifuged, and the supernatant was taken. The withdrawn supernatant was filtered and analyzed using a UV spectrophotometer and the amount of drug was calculated (5,33).…”

“…Transfersomes increase the elasticity of vesicles by redistribution of the edge activator and lipid in their milieu, whereas ethosomes act by fluidizing the lipids of both the skin as well as the vesicles (2)(3)(4)(5). In the present study, an attempt has been made for formulating transethosomes as novel vesicles containing both ethanol along with lipids, which mimic the properties of both transfersomes and ethosomes (9).…”

“…These elastic vesicles are of two types viz. transfersomes are composed of an edge activator and lipid, which are popularly known as transfersomes, and ethosomes are composed of lipid and ethanol (1)(2)(3)(4)(5)(6). These help in minimizing the washout of the drug through the blood, which is a common problem observed when drugs are given through the topical route using penetration enhancers, ionotophoresis, or electrophoresis mechanisms.…”